Atypical Neuroleptics Have Low Affinity for Dopamine D2 Receptors or Are Selective for D4 Receptors

Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction

1973 • 12,522 citations

Clozapine for the Treatment-Resistant Schizophrenic

1988 • 4,030 citations

Dopamine Receptor Binding Predicts Clinical and Pharmacological Potencies of Antischizophrenic Drugs

1976 • 2,224 citations

The membrane actions of anesthetics and tranquilizers.

1972 • 2,194 citations

Cloning of the gene for a human dopamine D4 receptor with high affinity for the antipsychotic clozapine

1991 • 2,008 citations

Antipsychotic drug doses and neuroleptic/dopamine receptors

1976 • 1,623 citations

Positron Emission Tomographic Analysis of Central D1 and D2 Dopamine Receptor Occupancy in Patients Treated With Classical Neuroleptics and Clozapine

1992 • 1,420 citations

Classification of typical and atypical antipsychotic drugs on the basis of dopamine D-1, D-2 and serotonin2 pKi values.

1989 • 1,313 citations

Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1

1991 • 1,157 citations

Cloning and expression of a rat D2 dopamine receptor cDNA

1988 • 1,125 citations

[3H]Ketanserin (R 41 468), a selective 3H-ligand for serotonin2 receptor binding sites. Binding properties, brain distribution, and functional role.

1982 • 1,049 citations

Multiple dopamine D4 receptor variants in the human population

1992 • 967 citations

Brain receptors for antipsychotic drugs and dopamine: direct binding assays.

1975 • 695 citations

Dopamine D4 receptors elevated in schizophrenia

1993 • 632 citations

Clinical studies on the mechanism of action of clozapine: the dopamine-serotonin hypothesis of schizophrenia

1989 • 600 citations

Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors

1994 • 592 citations

Antischizophrenic Drugs and Brain Cholinergic Receptors

1974 • 474 citations

Dopamine receptor sequences. Therapeutic levels of neuroleptics occupy D2 receptors, clozapine occupies D4.

1992 • 445 citations

IS IT POSSIBLE TO PREDICT THE CLINICAL EFFECTS OF NEUROLEPTIC DRUGS (MAJOR TRANQUILLIZERS) FROM ANIMAL DATA?I. "NEUROLEPTIC ACTIVITY SPECTRA" FOR RATS.

1965 • 348 citations

SPECT imaging of striatal dopamine release after amphetamine challenge.

1995 • 330 citations

The ratios of serotonin2 and dopamine2 affinities differentiate atypical and typical antipsychotic drugs.

1989 • 321 citations

Endogenous dopamine lowers the dopamine D₂ receptor density as measured by [³H]raclopride: Implications for positron emission tomography of the human brain

1989 • 298 citations

Effect of clozapine on the turnover of dopamine in the corpus striatum and in the limbic system

1973 • 296 citations

Striatal binding of the PET ligand ¹¹C‐raclopride is altered by drugs that modify synaptic dopamine levels

1993 • 285 citations

The behavioral pharmacology of olanzapine, a novel "atypical" antipsychotic agent.

1992 • 264 citations

Effects of antipsychotic drugs on serotonin receptors.

1991 • 260 citations

Regulation of transient dopamine concentration gradients in the microenvironment surrounding nerve terminals in the rat striatum

1992 • 258 citations

Antipsychotic agents antagonize non-competitiveN-methyl-d-aspartate antagonist-induced behaviors

1995 • 248 citations

Dopamine D4 receptor repeat: analysis of different native and mutant forms of the human and rat genes.

1994 • 238 citations

Membrane Stabilization by Drugs: Tranquilizers, Steroids, and Anesthetics

1966 • 234 citations

I. Erythrocyte membrane stabilization by tranquilizers and antihistamines

1966 • 224 citations

Serotonergic modulation of striatal dopamine measured with positron emission tomography (PET) and in vivo microdialysis

1995 • 216 citations

GABAergic inhibition of endogenous dopamine release measured in vivo with 11C-raclopride and positron emission tomography

1992 • 211 citations

Unique binding characteristics of antipsychotic agents interacting with human dopamine D2A, D2B, and D3 receptors.

1993 • 207 citations

Neuroleptic-induced hypersensitivity of striatal dopamine receptors in the rat as a model of tardive dyskinesias. Effects of clozapine, haloperidol, loxapine and chlorpromazine

1975 • 206 citations

Link between D1 and D2 dopamine receptors is reduced in schizophrenia and Huntington diseased brain.

1989 • 197 citations

Distribution of putative D4 dopamine receptors in postmortem striatum from patients with schizophrenia

1995 • 180 citations

Dopamine Receptor Parameters Detected by [³H]Spiperone Depend on Tissue Concentration: Analysis and Examples

1984 • 173 citations

Cooperativity Manifest in the Binding Properties of Purified Cardiac Muscarinic Receptors

1995 • 172 citations

Characterization of typical and atypical antipsychotic drugs based on in vivo occupancy of serotonin2 and dopamine2 receptors.

1993 • 170 citations

Nafadotride, a potent preferential dopamine D3 receptor antagonist, activates locomotion in rodents.

1995 • 164 citations

Amphetamine‐stimulated dopamine release competes in vivo for [¹²³I]IBZM binding to the D2 receptor in nonhuman primates

1992 • 157 citations

D2 dopamine receptor occupancy during low-dose treatment with haloperidol decanoate

1995 • 148 citations

Serotonergic involvement in haloperidol-induced catalepsy.

1993 • 144 citations

D4 dopamine receptor binding affinity does not distinguish between typical and atypical antipsychotic drugs

1995 • 143 citations

Full-length cDNA cloning and distribution of human dopamine D4 receptor

1995 • 141 citations

The displacement of membrane calcium by a local anesthetic (chlorpromazine)

1969 • 140 citations

Complete Conversion of Brain D₂ Dopamine Receptors from the High‐ to the Low‐Affinity State for Dopamine Agonists, Using Sodium Ions and Guanine Nucleotide

1985 • 139 citations

II. Erythrocyte membrane stabilization by local anesthetics and tranquilizers

1966 • 130 citations

Effects of central cholinergic blockade on striatal dopamine release measured with positron emission tomography in normal human subjects.

1993 • 128 citations

The surface activity of tranquilizers

1963 • 128 citations

8-hydroxy-2-(di-N-propylamino) tetralin, a selective serotonin1A receptor agonist, blocks haloperidol-induced catalepsy by an action on raphe nuclei medianus and dorsalis

1988 • 126 citations

Clozapine and N-desmethylclozapine are potent 5-HT1C receptor antagonists

1993 • 125 citations

Effects of endogenous dopamine on kinetics of [³H]N‐methylspiperone and [³H]raclopride binding in the rat brain

1991 • 122 citations

Dopamine D4 receptors and effects of guanine nucleotides on [3H]raclopride binding in postmortem caudate nucleus of subjects with schizophrenia or major depression

1995 • 121 citations

The effect of serotonergic agents on haloperidol-induced catalepsy

1990 • 118 citations

Clozapine is a partial agonist at cloned, human serotonin 5-HT1A receptors

1996 • 110 citations

Antipsychotic-like profile of combined treatment with raclopride and 8-OH-DPAT in the rat: enhancement of antipsychotic-like effects without catalepsy

1991 • 106 citations

An Exact Correction to the “Cheng-Prusoff” Correction

1988 • 105 citations

5-HT2 Antagonist Ritanserin in Neuroleptic-Induced Parkinsonism

1990 • 105 citations

Effects of endogenous dopamine on measures of [¹⁸F]N‐methylspiroperidol binding in the basal ganglia: Comparison of simulations and experimental results from PET studies in baboons

1991 • 105 citations

D2-Family receptor distribution in human postmortem tissue

1995 • 104 citations

Synaptic Concentration of Dopamine in the Mouse Striatum in Relationship to the Kinetic Properties of the Dopamine Receptors and Uptake Mechanism

1991 • 100 citations

Dopamine D1, D2 and serotonin2 receptor occupation by typical and atypical antipsychotic drugs in vivo.

1993 • 98 citations

Atypical neuroleptics: role of multiple receptors, endogenous dopamine, and receptor linkage

1990 • 96 citations

Amphetamine induced decreases in (¹⁸F)‐N‐methylspiroperidol binding in the baboon brain using positron emission tomography (PET)

1991 • 91 citations

Clozapine serum levels and side effects during steady state treatment of schizophrenic patients: a cross-sectional study

1995 • 87 citations

D1-, D2-, and 5-HT2-receptor occupancy in clozapine-treated patients.

1994 • 83 citations

Motor and mental aspects of extrapyramidal syndromes

1995 • 81 citations

Absence of detectable striatal dopamine D4 receptors in drug-treated schizophrenia

1995 • 81 citations

The Role of Serotonin in Schizophrenia and the Place of Serotonin-Dopamine Antagonist Antipsychotics

1995 • 77 citations

Deriving the therapeutic concentrations for clozapine and haloperidol: The apparent dissociation constant of a neuroleptic at the dopamine D2 or D4 receptor varies with the affinity of the competing radioligand

1995 • 73 citations

The Evolution of the Serotonin-Dopamine Antagonist Concept

1995 • 69 citations

Neuroleptic properties of cis-N-(1-benzyl-2-methylpyrrolidin-3-yl)-5-chloro-2-methoxy-4-methylaminobenzamide (YM-09151-2) with selective antidopaminergic activity

1981 • 65 citations

The cloned dopamine D2 receptor reveals different densities for dopamine receptor antagonist ligands. Implications for human brain positron emission tomography

1992 • 65 citations

Serotonergic and dopaminergic aspects of neuroleptic-induced extrapyramidal syndromes in nonhuman primates

1993 • 65 citations

Effect of metergoline, fenfluramine, and 8-OHDPAT on catalepsy induced by haloperidol or morphine

1988 • 63 citations

Antagonism by neuroleptics of serotonin 5-HT1A and 5-HT2 receptors of normal human brain in vitro

1987 • 63 citations

Pharmacological Actions of SM-9018, a New Neuroleptic Drug with Both Potent 5-Hydroxytryptamine2 and Dopamine2 Antagonistic Actions

1990 • 62 citations

Gaps and peculiarities in 5-HT2 receptor studies.

1990 • 62 citations

Schizophrenia: elevation of dopamine D4-like sites, using [3H]nemonapride and [125I]epidepride

1995 • 60 citations

Antagonism by 8-OH-DPAT, but not ritanserin, of catalepsy induced by SCH 23390 in the rat

1992 • 59 citations

Membrane expansion of the erythrocyte by both the neutral and ionized forms of chloropromazine

1969 • 57 citations

Plasma Clozapine Levels and the Treatment of L-DOPA-Induced Psychosis in Parkinson's Disease A High Potency Effect of Clozapine

1995 • 56 citations

Clozapine inhibits serotoninergic transmission by an action at α1-adrenoceptors not at 5-HT1A receptors

1994 • 54 citations

Interaction of psychotropic drugs with central 5-HT3 recognition sites: fact or artifact?

1989 • 52 citations

Cloning of two additional catecholamine receptors from rat brain

1990 • 51 citations

Amperozide – a new putatively antipsychotic drug with a limbic mode of action on dopamine mediated behaviour

1990 • 51 citations

Long-term haloperidol elevates dopamine D4 receptors by 2-fold in rats

1995 • 51 citations

Positron emission tomography with (18F)methylspiperone demonstrates D2 dopamine receptor binding differences of clozapine and haloperidol

1991 • 43 citations

Therapeutic receptor-blocking concentrations of neuroleptics

1995 • 39 citations

Dopamine and Serotonin Receptors: Amino Acid Sequences, and Clinical Role in Neuroleptic Parkinsonism

1996 • 39 citations

Regulation of Anterior Pituitary D₂ Dopamine Receptors by Magnesium and Sodium Ions

1985 • 39 citations

The effect of ritanserin on treatment-resistant neuroleptic induced akathisia: Case reports

1992 • 33 citations

Potential antipsychotic agents. 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds

1990 • 32 citations

The pharmacological properties of a potent neurotropic compound from the dibenzothiazepine group

1965 • 29 citations

Critical reevaluation of spiperone and benzamide binding to dopamine D2 receptors: evidence for identical binding sites

1996 • 28 citations

Pharmacological profile of the new potent neuroleptic ocaperidone (R 79,598).

1992 • 20 citations

Efficacy, safety, and dose response of three doses of sertindole and three doses of haldol in schizophrenic patients

1996 • 19 citations

Homovanillic acid in caudate and pre-frontal cortex following neuroleptics

1984 • 19 citations

Exogenous 1-dopa alters spiroperidol binding, , in the mouse striatum

1986 • 18 citations

Dopamine D-2 receptors in canine brain: ionic effects on [3H]neuroleptic binding

1987 • 17 citations

Plasma Clozapine Levels and the Treatment of L-DOPA-Induced Psychosis in Parkinson's Disease

1995 • 17 citations

Sterically hindered 5,11-dicarbo analogs of clozapine as potential chiral antipsychotic agents

1989 • 16 citations

SDZ GLC 756, a novel octahydrobenzo[g]quinoline derivative exerts opposing effects on dopamine D1 and D2 receptors

1996 • 16 citations

Bromperidol, a new butyrophenone neuroleptic: A review

1982 • 14 citations

pH dependence of sulpiride binding to D2 dopamine receptors in bovine brain

1991 • 14 citations

Motor and mental aspects of extrapyramidal syndromes

1995 • 13 citations

5HT2-receptor antagonists can attenuate submaximal haloperidol-induced catalepsy in rats

1995 • 13 citations

The dopamine D4 receptor in schizophrenia: an update

1996 • 13 citations

Distribution of dopamine D4 receptor in human postmortem brain sections: Autoradiographic studies with [3H]-NGD-94-1

1996 • 12 citations

Characterization of [3H]clozapine binding sites in rat brain

1995 • 11 citations

Long-term treatment with haloperidol or clozapine does not affect dopamine D4 receptors in rat frontal cortex

1995 • 11 citations

Stereospecific antidopaminergic and anticholinergic actions of the enantiomers of (+/-)-1-cyclopropylmethyl-4-(3-trifluoromethylthio-5H-dibenzo[a,d]cyclohepten-5-ylidene) piperidine (CTC), a derivative of cyproheptadine.

1979 • 10 citations

Chlorpromazine adsorption to brain regions

1971 • 10 citations

Two open-label, long-term safety studies of sertindole

1996 • 9 citations

Deriving the therapeutic concentrations for clozapine and haloperidol: The apparent dissociation constant of a neuroleptic at the dopamine D2 or D4 receptor varies with the affinity of the competing radioligand

1995 • 7 citations

Therapeutic receptor-blocking concentrations of neuroleptics

1995 • 6 citations

Dopamine D2, D3, D4 receptors in human postmortem brain sections: Comparison between normals and schizophrenics

1996 • 5 citations

The serotonin-dopamine interaction measured with positron emission tomography (PET) and C-11 raclopride in normal human subjects

1994 • 3 citations

Distinct localization and regulation of dopamine D3 receptors: Autoradiographic studies

1995 • 3 citations

Systemic and intracortical administration of ritanserin increases in vivo dopamine release in rat prefrontal corteX

1995 • 3 citations

Dopamine D2-like receptors are elevated after chronic treatment with typical and atypical neuroleptics

1995 • 1 citations